CNS Stimulants Flashcards
(27 cards)
Examples of Catecholamine releasers
Amphetamine (Adderal)
Methamphetamine (better CNS access than amphetamine)
Methylphenidate (Ritalin)
Ephedrine (decong. + alpha nad beta ag)
Four ways that a catacholamine releaser may work
- Binds to presynaptic membrane and induces vasicle release
- Causes DA release from vesicles into the intracellular space/terminal (VMAT)
- Blocks MAO, blocking degradation of DA, causing buildup inside cytoplasm in terminal
- Induces reverse transport thrrouh DAT to release DA into EC space
Effects of Cocaine
Pure block of reuptake, prolonging lifetime catecholaine in the synapse, promoting action on post-synaptic cell
NaV Activity
Important details on Modafinil
Monamine reuptake blocker
MOA unclear
Less abuse potetial
What are bath salts?
Cathinones – naturally occuring psychostimulants. commonly abused.
- Mechanisms differ
- Intox: psychosis, agitation/violence, tachy, HTN, hyperthermia
- Schedule 1 drugs
Effects of MDPV
Reuptake blocker for DAT and NET (10-50x cocaine potency)
Important details on Atomoxetine
NET activity
Alternate treatment for refractory ADHD/ADD, Adult ADD
Importnat details on buproprion
Mild NET and DAT blocker + nAChR antagonist
Treats depression + nicotine cessation
Main methylxanthines
Caffeine
Theophylline (asthma)
Theobromine
Theory for how caffeine works
Antagonist of adenosine receptor
Adensine triggers inhibition of NT release and blocks post synatptic effects
Details on Nicotinic acetylcholine recepotrs
ACh gated cation channels where activation promotes cellular depolarization and neurotransmitter release hen receptors on presynaptic terminals are activated
Effects of Nicotine in DA system
Stimulate AP firing
Stimulate DA release (direct and indirect)
Difference btw Nicotine and ACh
ACh is endogenous. Nicotine is also very similar to local anesthetics. ACh doesn’t get protenated, doesn’t get into membrane very easily. Natural presence of actylcholinesterase to keep ACh under control.
Difference between free base and singly protenated nicotine
free is a membrane crosser
singly can activate
structural similarities with ACh and Nicotine
Nitrogens that are protenated at physiological pH
Hydrogen bond acceptors
Important details on Varenacline
Partial agonist of nAChRs (a4b2)
effects on a3b4 nAChRs may cause periphera side effects
Toxicities of Amphetamines
CV – HTN, tachy
Psych – psychosis
Toxicities of Cocaine
CV - MI, stroke, arrythmias
CNS - Seizures
Respiratory Depression
Toxicities of Nicotinics
GI upset
Odd dreams + suicidal ideations
Stimulants used to treat ADHD
Amphetamine (Adderall)
Methylphenidate (Ritalin)
Adcerse effects of amphetamine/methylphenidate treatment
Insomnia
Ab. Pian
Anorexia/Weight Loss
Growth Suppression in Kids
Describe Narcolepsy
Refreshing sleep attacks
Cataplexy
REM sleep intrusions
What is cataplexy
Sudden loss of muscle tone (bilateral) often associated with intense emotional engagement
Tx for narcolepsy
TCAs and MAOIs
Methylphenidate, Amphetamine
Modafinil (less dependence)
